Overview

NCI Definition [1]:
An orally available, reversible, noncompetitive inhibitor of lysine-specific demethylase 1 (LSD1, or KDM1A), with potential antineoplastic activity. Upon oral administration, seclidemstat reversibly inhibits LSD1, a demethylase that suppresses the expression of target genes by converting the di- and mono-methylated forms of lysine at position 4 of histone 3 (H3K4) to mono- and unmethylated H3K4, respectively. LSD1 inhibition enhances H3K4 methylation and increases the expression of tumor suppressor genes. This may lead to an inhibition of cell growth in LSD1-overexpressing tumor cells. In addition, LSD1 demethylates mono- or di-methylated H3K9 which increases gene expression of tumor promoting genes; inhibition of LSD1 promotes H3K9 methylation and decreases transcription of these genes.

Seclidemstat has been investigated in 4 clinical trials, of which 4 are open and 0 are closed. Of the trials investigating seclidemstat, 3 are phase 1 (3 open) and 1 is phase 1/phase 2 (1 open).

ARID1A Loss, ARID1A Mutation, and ASXL1 Loss are the most frequent biomarker inclusion criteria for seclidemstat clinical trials.

Chronic myelomonocytic leukemia-0, chronic myelomonocytic leukemia-1, and chronic myelomonocytic leukemia-2 are the most common diseases being investigated in seclidemstat clinical trials [2].

Top Biomarker Inclusion Criteria for Open Clinical Trials Investigating Seclidemstat
This graph displays the 20 most frequently occurring biomarkers curated on clinical trials investigating seclidemstat and the cancer types associated with these biomarkers. These numbers are derived from a set of 5,956 clinical trials for which biomarker status defines treatment.

Drug Details

Synonyms [2]:
sp2577, sp-2577, sp 2577, seclidemstat, lsd1 inhibitor sp-2577
Drug Target(s) [2]:
KDM1A
NCIT ID [1]:
C154328

References

1. National Cancer Institute. NCI Thesaurus Version 18.11d. https://ncit.nci.nih.gov/ncitbrowser/. [2018-07-30] [2018-08-02].

2. All assertions and clinical trial landscape data are curated from primary sources. You can read more about the curation process here.